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Bioorg Med Chem Lett. 2009 Apr 15;19(8):2172-5. doi: 10.1016/j.bmcl.2009.02.110. Epub 2009 Mar 3.

Fluorinated non-imidazole histamine H3 receptor antagonists.

Author information

Johann Wolfgang Goethe-Universität, Institut für Pharmazeutische Chemie, Biozentrum, ZAFES/LiFF/CMP, Frankfurt, Germany.

Erratum in

  • Bioorg Med Chem Lett. 2009 Jun 15;19(12):3348. Galaparti, A [corrected to Garlapati, A].


Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (piperidine or pyrrolidine) and are fluoro substituted in different positions of the basic alicyclic moiety. Pharmacological evaluation resulted in ligands with high affinities at hH(3) receptor in the nanomolar and subnanomolar concentration range and some with high antagonist in vivo potencies.

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